Hidtil ukendte cephalotaxan-derivater og fremgangsmåde til fremstilling deraf

The present invention concerns a new general process for asymmetric hemisynthesis of harringtonines and their analogs, that are alkaloids used in chemotherapy. This process comprises direct esterification of a natural cephalotaxine with an acylating compound constituted of a side chain precursor whi...

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Hauptverfasser: CHAUVIAT, LUDOVIC, POUTOT, SANDRINE, ROBIN, JEAN-PIERRE, CHARBONNEL, SANDRA, DHAL, ROBERT, GIRODIER, LAURENT, GILET, CHRYSTELLE, DUJARDIN, GILLES, ROBIN, JULIE, ROUAUD, SYLVIE, CAVOLEAU, SYLVIE, MEVELEC, LAURENCE, FOURNIER, FLORENCE
Format: Patent
Sprache:dan
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Zusammenfassung:The present invention concerns a new general process for asymmetric hemisynthesis of harringtonines and their analogs, that are alkaloids used in chemotherapy. This process comprises direct esterification of a natural cephalotaxine with an acylating compound constituted of a side chain precursor which backbone and functionalization are entirely preformed. The invention also concerns a natural, synthetic or semi-synthetic harringtonines including their tautomeric forms and their salts of the following formula: wherein n=2 (i.e. harringtonine) or n=3 (i.e. homoharringtonine), in which the total content of impurities, possibly including enantiomeric forms, is lower than 1%, and/or the content of the major impurity is lower than 0.9%, and/or the chromatographic assay exhibits a harringtonines content higher than 97.5%.